EP3517535A4 - Composé hétérocyclique substitué par un alcynyle, son procédé de préparation et son utilisation médicale - Google Patents

Composé hétérocyclique substitué par un alcynyle, son procédé de préparation et son utilisation médicale Download PDF

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Publication number
EP3517535A4
EP3517535A4 EP17849992.7A EP17849992A EP3517535A4 EP 3517535 A4 EP3517535 A4 EP 3517535A4 EP 17849992 A EP17849992 A EP 17849992A EP 3517535 A4 EP3517535 A4 EP 3517535A4
Authority
EP
European Patent Office
Prior art keywords
alkynyl
preparation
heterocyclic compound
substituted heterocyclic
method therefor
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP17849992.7A
Other languages
German (de)
English (en)
Other versions
EP3517535A1 (fr
EP3517535B1 (fr
Inventor
Xiangyang Chen
Yingxiang GAO
Norman Xianglong Kong
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Beijing Innocare Pharma Tech Co Ltd
Original Assignee
Beijing Innocare Pharma Tech Co Ltd
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Filing date
Publication date
Application filed by Beijing Innocare Pharma Tech Co Ltd filed Critical Beijing Innocare Pharma Tech Co Ltd
Publication of EP3517535A1 publication Critical patent/EP3517535A1/fr
Publication of EP3517535A4 publication Critical patent/EP3517535A4/fr
Application granted granted Critical
Publication of EP3517535B1 publication Critical patent/EP3517535B1/fr
Active legal-status Critical Current
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP17849992.7A 2016-09-19 2017-01-25 Composé hétérocyclique substitué par un alcynyle, son procédé de préparation et son utilisation médicale Active EP3517535B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610833890.3A CN107840842A (zh) 2016-09-19 2016-09-19 炔代杂环化合物、其制备方法及其在医药学上的应用
PCT/CN2017/072570 WO2018049781A1 (fr) 2016-09-19 2017-01-25 Composé hétérocyclique substitué par un alcynyle, son procédé de préparation et son utilisation médicale

Publications (3)

Publication Number Publication Date
EP3517535A1 EP3517535A1 (fr) 2019-07-31
EP3517535A4 true EP3517535A4 (fr) 2020-02-26
EP3517535B1 EP3517535B1 (fr) 2022-06-29

Family

ID=61618562

Family Applications (1)

Application Number Title Priority Date Filing Date
EP17849992.7A Active EP3517535B1 (fr) 2016-09-19 2017-01-25 Composé hétérocyclique substitué par un alcynyle, son procédé de préparation et son utilisation médicale

Country Status (12)

Country Link
US (3) US10710981B2 (fr)
EP (1) EP3517535B1 (fr)
JP (1) JP6906811B2 (fr)
KR (1) KR20190052113A (fr)
CN (2) CN107840842A (fr)
AU (1) AU2017327954B2 (fr)
CA (1) CA3036594C (fr)
ES (1) ES2925212T3 (fr)
MX (1) MX2019003143A (fr)
RU (1) RU2729069C1 (fr)
SG (1) SG10202102822RA (fr)
WO (1) WO2018049781A1 (fr)

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WO2020120673A1 (fr) * 2018-12-13 2020-06-18 Intervet International B.V. Procédé de préparation de 1-[(3r,4s)-4-cyanotétrahydropyran-3-yl]-3-[(2-fluoro-6-méthoxy-4-pyridyl)amino]pyrazole-4-carboxamide
CN113474337A (zh) 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3，5-二甲氧基苯基)氨基)喹喔啉衍生物
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
AU2020378630A1 (en) 2019-11-08 2022-05-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
AU2020412067A1 (en) * 2019-12-26 2022-08-11 Beijing Innocare Pharma Tech Co., Ltd. Crystalline forms of (S) -1- (1-acryloylpyrrolidin-3-yl) -3- ( (3, 5-dimethoxyphenyl) ethynyl) -5- (methylamino) -1H-pyrazole-4-carboxamide
WO2021148581A1 (fr) 2020-01-22 2021-07-29 Onxeo Nouvelle molécule dbait et son utilisation
WO2021247971A1 (fr) * 2020-06-05 2021-12-09 Kinnate Biopharma Inc. Inhibiteurs des kinases du récepteur du facteur de croissance des fibroblastes
US11345681B1 (en) * 2020-06-05 2022-05-31 Kinnate Biopharma Inc. Inhibitors of fibroblast growth factor receptor kinases
JP2024503661A (ja) * 2021-01-12 2024-01-26 ベイジン・イノケア・ファーマ・テク・カンパニー・リミテッド （ｓ）－１－（１－アクリロイルピロリジン－３－イル）－３－（（３，５－ジメトキシフェニル）エチニル）－５－（メチルアミノ）－１ｈ－ピラゾール－４－カルボキサミドの製造方法
CN115433190A (zh) * 2021-06-02 2022-12-06 药雅科技(上海)有限公司 不可逆杂环化合物fgfr抑制剂的制备方法和用途
CN114853739B (zh) * 2021-02-03 2023-09-22 药雅科技(上海)有限公司 一种炔代吡嗪类fgfr抑制剂及其制备方法和用途
CN115043832B (zh) * 2021-03-08 2023-08-22 药雅科技(上海)有限公司 一种fgfr抑制剂炔代杂环类化合物及其制备方法和用途
MX2024005341A (es) * 2021-11-03 2024-05-20 Beijing Innocare Pharma Tech Co Ltd Dispersion solida amorfa que comprende (s)-1-(1-acriloilpirrolidin -3-il)-3-((3,5-dimetoxifenil)etinil)-5-(metilamino)-1h-pirazol-4- carboxamida.
CN118354772A (zh) * 2021-11-16 2024-07-16 北京诺诚健华医药科技有限公司 治疗头颈癌的方法
WO2023107980A1 (fr) * 2021-12-08 2023-06-15 Kinnate Biopharma Inc. Formes à l'état solide d'un inhibiteur de fgfr
CA3240059A1 (fr) * 2021-12-08 2023-06-15 Kinnate Biopharma Inc. Traitement du cancer avec un inhibiteur de la kinase fgfr
WO2023107870A1 (fr) * 2021-12-08 2023-06-15 Kinnate Biopharma Inc. Inhibiteurs des kinases du récepteur du facteur de croissance des fibroblastes

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EP3023100A1 (fr) * 2013-07-18 2016-05-25 Taiho Pharmaceutical Co., Ltd. Médicament antitumoral pour l'administration intermittente d'inhibiteur de fgfr

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EP3023100A1 (fr) * 2013-07-18 2016-05-25 Taiho Pharmaceutical Co., Ltd. Médicament antitumoral pour l'administration intermittente d'inhibiteur de fgfr

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Also Published As

Publication number Publication date
US11572353B2 (en) 2023-02-07
AU2017327954A1 (en) 2019-05-02
AU2017327954B2 (en) 2022-02-03
RU2729069C1 (ru) 2020-08-04
US11059805B2 (en) 2021-07-13
CN109843873B (zh) 2022-06-17
CA3036594A1 (fr) 2018-03-22
US20190210997A1 (en) 2019-07-11
EP3517535A1 (fr) 2019-07-31
JP2019529444A (ja) 2019-10-17
CN107840842A (zh) 2018-03-27
US20210332027A1 (en) 2021-10-28
JP6906811B2 (ja) 2021-07-21
WO2018049781A1 (fr) 2018-03-22
US20200339541A1 (en) 2020-10-29
CN109843873A (zh) 2019-06-04
EP3517535B1 (fr) 2022-06-29
ES2925212T3 (es) 2022-10-14
MX2019003143A (es) 2019-06-17
SG10202102822RA (en) 2021-05-28
KR20190052113A (ko) 2019-05-15
CA3036594C (fr) 2024-02-13
US10710981B2 (en) 2020-07-14

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